Discovery of a Covalent Inhibitor of KRAS^G12C (AMG 510) for the Treatment of Solid Tumors

Brian A. Lanman, Jennifer R. Allen, John G. Allen, +41

Journal of Medicinal Chemistry

Drug TargetSolid TumorsMolecular BiologyCryptic PocketChemical Biology +18

Discovery and Optimization of a Series of Benzothiazole Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitors

Noel D. D’Angelo, Tae‐Seong Kim, Kristin L. Andrews, +25

Journal of Medicinal Chemistry

Drug TargetPharmacotherapyBenzothiazole Phosphoinositide 3-KinaseChemical BiologyPharmaceutical Chemistry +19

Discovery of <i>N</i>-(1-Acryloylazetidin-3-yl)-2-(1<i>H</i>-indol-1-yl)acetamides as Covalent Inhibitors of KRAS^G12C

Youngsook Shin, Joon Won Jeong, Ryan P. Wurz, +24

ACS Medicinal Chemistry Letters

Structure-Based Design of Novel Class II c-Met Inhibitors: 2. SAR and Kinase Selectivity Profiles of the Pyrazolone Series

Longbin Liu, Mark H. Norman, Matthew Lee, +16

Journal of Medicinal Chemistry

Drug TargetChemical BiologyPharmaceutical ChemistryTumor BiologyDrug Resistance +19

Chloroquine treatment induces secretion of autophagy-related proteins and inclusion of Atg8-family proteins in distinct extracellular vesicle populations

Jing Xu, Kevin Yang, Nancy E. Go, +8

Autophagy

Outcomes of pancreaticoduodenectomy for pancreatic malignancy in octogenarians: an American College of Surgeons National Surgical Quality Improvement Program analysis

David Y. Lee, Jamie A. Schwartz, Barbara Wexelman, +3

The American Journal of Surgery

Surgical OncologyPancreatic CancerAmerican CollegeOutcomes ResearchPancreatic Malignancy +3

Phospshoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitors: Discovery and Structure–Activity Relationships of a Series of Quinoline and Quinoxaline Derivatives

Nobuko Nishimura, Aaron Siegmund, Longbin Liu, +19

Journal of Medicinal Chemistry

Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 3. Structure–Activity Relationships within the Aryl Carbinol Region of the <i>N</i>-Arylsulfonamido-<i>N</i>′-arylpiperazine Series

Nobuko Nishimura, Mark H. Norman, Longbin Liu, +17

Journal of Medicinal Chemistry

Molecular BiologyChemical BiologyStructure–activity RelationshipsInsulin SignalingMolecular Pharmacology +20

A new quinoline-based chemical probe inhibits the autophagy-related cysteine protease ATG4B

Damien Bosc, Lubomir Vezenkov, Svetlana Bortnik, +21

Scientific Reports

Selective Class I Phosphoinositide 3-Kinase Inhibitors: Optimization of a Series of Pyridyltriazines Leading to the Identification of a Clinical Candidate, AMG 511

Mark H. Norman, Kristin L. Andrews, Yunxin Bo, +34

Journal of Medicinal Chemistry

Chemoprevention StrategyMolecular BiologyClinical CandidatePharmacotherapyChemical Biology +17